Voltage-gated rearrangements associated with differential beta-subunit modulation of the L-type Ca(2+) channel inactivation

Biophys J. 2004 Aug;87(2):844-57. doi: 10.1529/biophysj.104.041152.

Abstract

Auxiliary beta-subunits bound to the cytoplasmic alpha(1)-interaction domain of the pore-forming alpha(1C)-subunit are important modulators of voltage-gated Ca(2+) channels. The underlying mechanisms are not yet well understood. We investigated correlations between differential modulation of inactivation by beta(1a)- and beta(2)- subunits and structural responses of the channel to transition into distinct functional states. The NH(2)-termini of the alpha(1C)- and beta-subunits were fused with cyan or yellow fluorescent proteins, and functionally coexpressed in COS1 cells. Fluorescence resonance energy transfer (FRET) between them or with membrane-trapped probes was measured in live cells under voltage clamp. It was found that in the resting state, the tagged NH(2)-termini of the alpha(1C)- and beta-subunit fluorophores are separated. Voltage-dependent inactivation generates strong FRET between alpha(1C) and beta(1a) suggesting mutual reorientation of the NH(2)-termini, but their distance vis-à-vis the plasma membrane is not appreciably changed. These voltage-gated rearrangements were substantially reduced when the beta(1a)-subunit was replaced by beta(2). Differential beta-subunit modulation of inactivation and of FRET between alpha(1C) and beta were eliminated by inhibition of the slow inactivation. Thus, differential beta-subunit modulation of inactivation correlates with the voltage-gated motion between the NH(2)-termini of alpha(1C)- and beta-subunits and targets the mechanism of slow voltage-dependent inactivation.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • COS Cells
  • Calcium Channels, L-Type / chemistry
  • Calcium Channels, L-Type / physiology*
  • Cell Line
  • Chlorocebus aethiops
  • Fluorescence Resonance Energy Transfer / methods
  • Humans
  • Ion Channel Gating / physiology*
  • Kidney / chemistry
  • Kidney / embryology
  • Kidney / physiology*
  • Membrane Potentials / physiology*
  • Patch-Clamp Techniques / methods
  • Protein Subunits / chemistry
  • Protein Subunits / metabolism*
  • Recombinant Proteins / metabolism
  • Statistics as Topic
  • Structure-Activity Relationship

Substances

  • Calcium Channels, L-Type
  • L-type calcium channel alpha(1C)
  • Protein Subunits
  • Recombinant Proteins